HC-067047|cas:883031-03-6|西域试剂

HC-067047,99.78%

产品编号：Bellancom-100208| CAS NO：883031-03-6| 分子式：C₂₆H₂₈F₃N₃O₂| 分子量：471.51

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-100208	￥660.00	杭州北京（现货）
Bellancom-100208	￥1100.00	杭州北京（现货）
Bellancom-100208	￥2265.00	杭州北京（现货）
Bellancom-100208	￥4300.00	杭州北京（现货）
Bellancom-100208	￥7700.00	杭州北京（现货）

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HC-067047

产品介绍

HC-067047 是一种有效的选择性 TRPV4 拮抗剂，可逆地抑制流经人，大鼠和小鼠 TRPV4 直系同源物的电流，IC₅₀ 值分别为 48 nM，133 nM 和 17 nM。

生物活性

HC-067047 is a potent and selective TRPV4 antagonist and reversibly inhibits currents through the human, rat, and mouse TRPV4 orthologs with IC₅₀ values of 48 nM, 133 nM, and 17 nM, respectively.

体外研究

HC-067047 (1 µM; 24 hours; HEI-OC1 cells) treatment significantly decreases mRNA expression in high glucose cultured HEI-OC1 cells.
HC-067047 (1 µM; 24 hours; HEI-OC1 cells) treatment significantly decreases the expression of TRPV4 protein.
HC-067047 (1 µM; 48 hours; HEI-OC1 cells) treatment inhibits cell proliferation.
HC-067047 (1 µM; 48 hours; HEI-OC1 cells) treatment promotes cell apoptosis.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

RT-PCR

Cell Line:	HEI-OC1 cells
Concentration:	1 µM
Incubation Time:	24 hours
Result:	The mRNA expression was significantly decreased.

Western Blot Analysis

Cell Line:	HEI-OC1 cells
Concentration:	1 µM
Incubation Time:	24 hours
Result:	The expression of TRPV4 protein was significantly decreased.

Cell Proliferation Assay

Cell Line:	HEI-OC1 cells
Concentration:	1 µM
Incubation Time:	48 hours
Result:	Inhibited cell proliferation.

Apoptosis Analysis

Cell Line:	HEI-OC1 cells
Concentration:	1 µM
Incubation Time:	48 hours
Result:	Promoted cell apoptosis.

体内研究
(In Vivo)

HC-067047 (0-50 mg/kg; intraperitoneal injection; for 30 minutes; cyclophosphamide-treated WT and Trpv4^−/− mice, and naive WT mice) treatment increases functional bladder capacity and reduces micturition frequency in WT mice with cystitis. HC-067047 do not affect bladder function in Trpv4^−/− mice.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Cyclophosphamide-treated WT and Trpv4^−/− mice, and naive WT mice
Dosage:	0 mg/kg, 1 mg/kg, 10 mg/kg, 50 mg/kg
Administration:	Intraperitoneal injection; for 30 minutes
Result:	Increased functional bladder capacity and reduces micturition frequency in WT mice with cystitis and did not affect bladder function in Trpv4^−/− mice.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Cyclophosphamide-treated WT and Trpv4^−/− mice, and naive WT mice
Dosage:	0 mg/kg, 1 mg/kg, 10 mg/kg, 50 mg/kg
Administration:	Intraperitoneal injection; for 30 minutes
Result:	Increased functional bladder capacity and reduces micturition frequency in WT mice with cystitis and did not affect bladder function in Trpv4^−/− mice.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Cyclophosphamide-treated WT and Trpv4^−/− mice, and naive WT mice
Dosage:	0 mg/kg, 1 mg/kg, 10 mg/kg, 50 mg/kg
Administration:	Intraperitoneal injection; for 30 minutes
Result:	Increased functional bladder capacity and reduces micturition frequency in WT mice with cystitis and did not affect bladder function in Trpv4^−/− mice.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (106.04 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1208 mL	10.6042 mL	21.2085 mL
5 mM	0.4242 mL	2.1208 mL	4.2417 mL
10 mM	0.2121 mL	1.0604 mL	2.1208 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (5.30 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.30 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (5.30 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.30 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.30 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.30 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。